Tianeptine for Social Anxiety: Effective with Few Side Effects

Tianeptine is useful for social anxiety for many reasons. It has a favorable side effect profile. Unlike other drugs prescribed for anxiety like benzodiazepines, it’s non-impairing. Tianeptine also elevates mood. Increased positive affect seems to improve social interactions. (Or conversely, if you’re obviously depressed, it can make for some uncomfortable social encounters.)

In the United States, tianeptine is an unconventional treatment because it’s not FDA approved. Tianeptine is a potent tricyclic antidepressant that must be prescribed by a doctor in Europe. Tianeptine is in a legal grey area in the US, because it’s marketed and sold as a nootropic or nutraceutical. But it’s a potent drug that should probably be prescribed rather than purchased over-the-counter.

How Social Anxiety Develops

Individuals with social anxiety (SA) are invested in the impression that they make. They place a large importance on being socially appraised in a positive light. SA often involves over-activation of the sympathetic response or hypervigilence in social situations. High-anxiety individuals tend to over-focus on themselves and are sensitized to social signals. This state of enhanced sensitivity can impair social performance.

Social anxiety (SA) can be debilitating. Yet, there are some overlooked positive aspects to SA. Individuals with SA are more attentive to other peoples states of mind. One study reported enhanced empathy in high-SA individuals. More anxious states increase awareness of the environment and help in reading social cues. But excessive sensitivity to social signals can also impair social behavior.

Benefits of Tianeptine for Social Anxiety

Tianeptine has grown in popularity over the last five years. It’s now a bestselling product at nootropics vendors.

There are good reasons to think that tianeptine alleviates social anxiety.

The mood-elevating effects of tianeptine are helpful if low mood makes social interactions uncomfortable.

Tianeptine is an opioid, and opioids have anti-anxiety (anxiolytic) effects

Unlike benzodiazepines, Tianeptine is non-impairing

Tianeptine reverses stress-induced changes in the brain that may hinder social cognition

Anecdotal reports about the use if tianeptine for SA have been favorable

Tianeptine Risks

There are some disadvantages to tianeptine.

Tianeptine has a rapid half-life and only lasts 3 hours. Tianeptine’s rate of elimination may thus require re-dosing throughout the day. Case reports have described tianeptine dependence, abuse and withdrawal. Tianeptine activates the mu-opioid receptor in the brain. Painkillers like oxycodone are also mu-opioid agonists. Opioids are some of the most widely abused substances.

But tianeptine does not carry the same abuse potential as many other opioids. Tianeptine’s recreational potential is limited. Excessive dosages only result in a mild “high” without euphoria. The typical dosage is 12.5mg – 25mg.

Tianeptine vs Other Anti-Anxiety Medications

Benzodiazepines like Xanax – affect GABA, the major inhibitory neurotransmitter

SSRIs like Zoloft – increase concentrations of serotonin at the synapse (connection between neurons)

MAOIs like Parnate – Increase serotonin, norepinephrine, and dopamine by inhibiting their metabolism

Antihistamines like Remeron – block the histamine receptor and the serotonin 5HT2A receptor. Remeron also disinhibits serotonin and norepinephrine release

Atypical antipsychotics like Risperidone

From the laundry list of drugs above, it’s easy to see that there’s no magic bullet for SA. Many of these drugs have major side effects.

Benzodiazepines predispose to memory loss and cognitive impairment. SSRIs cause sexual dysfunction and in some cases actually exacerbate SA. A study hypothesized that too much serotonin (rather than too little as thought before) contributes to SA.

MAOIs are considered effective even for treatment resistant SA. Phenelzine affects both GABA (by inhibiting GABA transaminase), as well as monoamines. The side effects of this class of medication are serious, but overstated. Fears about a hypertensive crisis from consuming tyramine are overblown. While it is necessary to restrict tyramine, carrying nifedipine reduces the risk of a crisis. Nifedipine is a powerful and rapid-acting blood pressure lowering medication.

In contrast to these well-known medications used to treat SA, tianeptine is unknown by physicians in the US. Tianeptine’s mechanism is poorly understood, making it difficult to compare it to other drugs. The most important discovery about tianeptine is it’s binding affinity for mu-opioid receptors.

All considered, tianeptine is an effective and well-tolerated medication for SA. It also has potential to restore brain function after severe and chronic stress. But tianeptine has the disadvantage of being unknown by physicians outside of Europe. This lack of physician oversight leads individuals with SA to self-medicate, which is not ideal.

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